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Lapatinib

Phase 3

Breast Cancer | Small molecule | Oncology |Roche Holding AG|Last Updated: May 6, 2023

Success Probability

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Market & Valuation

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Trial Design

RandomizedACTIVE_CONTROLLEDDMC
Total Trials2
Total Enrollment1,342

FDA Designations

No designations recorded

Clinical trial landscape

Lapatinib · 2 trials · 1 indication

Phase 3 2
NCT03084939Efficacy and Safety of Trastuzumab Emtansine in Chinese Participants With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Locally Advanced or Metastatic Breast CancerBreast Cancer
COMPLETED351 Analytics
NCT00829166A Study of Trastuzumab Emtansine Versus Capecitabine + Lapatinib in Participants With HER2-positive Locally Advanced or Metastatic Breast CancerBreast Cancer
COMPLETED991 Analytics
PHASE3COMPLETED
Efficacy and Safety of Trastuzumab Emtansine in Chinese Participants With Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Locally Advanced or Metastatic Breast Cancer
Breast CancerUnlock trial analytics
PHASE3COMPLETED
A Study of Trastuzumab Emtansine Versus Capecitabine + Lapatinib in Participants With HER2-positive Locally Advanced or Metastatic Breast Cancer
Breast CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Progression-free survival (PFS)
Up to approximately 17 months

PFS is defined as the time from randomization to the first occurrence of disease progression as determined by the investigator using Response Evaluation Criteria in Solid Tumors (RECIST) Version (v1.1), or death from any cause during the study, whichever occurs first. Disease progression is defined as at least a 20% increase in the sum of diameters of target lesions with an absolute increase of at least 5 millimeter (mm) taking as reference the smallest sum during the study including baseline or the appearance of one or more new lesions. Tumor assessments will be performed with computed tomography (CT) or magnetic resonance imaging (MRI) scans.

Percentage of Participants With PD or Death as Assessed by an Independent Review Committee (IRC)
From the date of randomization through the data cut-off date of 14 Jan 2012 (up to 2 years, 11 months)

PD was assessed by an IRC using modified Response Evaluation Criteria in Solid Tumors (RECIST). All measurable lesions up to a maximum of 5 per organ and 10 in total were identified as target lesions (TLs) and recorded at baseline. TLs should be selected on the basis of their size (those with the longest diameter) and their suitability for accurate repeated measurements either by imaging or clinically. A sum of the longest diameter for all TLs was calculated as baseline sum longest diameter (SLD). All other lesions (or sites of disease) should be identified as non-TLs and recorded at baseline. PD for TLs was defined as greater than or equal to (\>/=) 20 percent (%) increase in SLD, taking as reference smallest SLD recorded since treatment started or appearance of 1 or more new lesions. PD for non-TLs was defined as appearance of 1 or more new lesions and/or unequivocal progression of existing non-TLs. Percentage of Participants with PD by IRC or death from any cause was reported.

Progression-free Survival (PFS) as Assessed by an IRC (Co-primary Endpoint)
From the date of randomization through the data cut-off date of 14 Jan 2012 (up to 2 years, 11 months)

Tumor response was assessed by an IRC according to modified RECIST. All measurable lesions up to a maximum of 5 per organ and 10 in total were identified as TLs (on the basis of their size and their suitability for accurate repeated measurements either by imaging or clinically) and recorded at baseline. A sum of the longest diameter for all TLs was calculated as baseline SLD. All other lesions were identified as non-TLs and recorded at baseline. PD for TLs: \>/= 20% increase in the SLD, taking as reference the smallest SLD recorded since treatment started or appearance of 1 or more new lesions. PD for non-TLs: appearance of 1 or more new lesions and/or unequivocal progression of existing non-TLs. PFS: time from randomization to first documented PD by IRC or death from any cause (whichever occurred earlier). The median duration of PFS was estimated using Kaplan-Meier method. The 95% confidence interval (CI) was computed using the method of Brookmeyer and Crowley.

Percentage of Participants Who Died: Second Interim Analysis
From the date of randomization through the data cut-off date of 31 Jul 2012 (up to 3 years, 5 months)

The percentage of participants who died from any cause was reported. The results are reported from second interim analysis, which deemed to be the confirmatory.

Overall Survival: Second Interim Analysis (Co-primary Endpoint)
From the date of randomization through the data cut-off date of 31 Jul 2012 (up to 3 years, 5 months)

OS was defined as the time from the date of randomization to the date of death from any cause. The median duration of OS was estimated using Kaplan-Meier method. The 95% CI was computed using the method of Brookmeyer and Crowley. The results are reported from second interim analysis, which deemed to be the confirmatory.

Percentage of Participants Who Died: Final Analysis
From the date of randomization through the data cut-off date of 31 Dec 2014 (up to 5 years, 11 months)

The percentage of participants who died from any cause was reported. The results reported are from the final analysis. The final analysis is descriptive.

Overall Survival: Final Analysis
From the date of randomization through the data cut-off date of 31 Dec 2014 (up to 5 years, 11 months)

OS was defined as the time from the date of randomization to the date of death from any cause. The median duration of OS was estimated using Kaplan-Meier method. The 95% CI was computed using the method of Brookmeyer and Crowley. The results reported are from the final analysis. The final analysis is descriptive.

Percentage of Participants Who Were Alive at Year 1
Year 1

1 year survival was defined as the percentage of participants alive 1 year after starting treatment. The results reported are from the final analysis.

Percentage of Participants Who Were Alive at Year 2
Year 2

2 year survival was defined as the percentage of participants alive 2 years after starting treatment. The results reported are from the final analysis.

Secondary Endpoints

Objective Response Rate (ORR)
Up to approximately 29 months
Duration of Response (DOR)
Up to approximately 29 months
Overall Survival (OS)
When at least 100 (50%) death events are observed from participants in Stage 1
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Trastuzumab EmtansineEXPERIMENTALParticipants with HER2-positive, unresectable LABC or MBC who have experienced disease progression after treatment with trastuzumab and a taxane will be treated with trastuzumab emtansine. Participants may continue to receive study treatment until disease progression (as assessed by the investigator), unmanageable toxicity, or study termination by the Sponsor.
Control (lapatinib + capecitabine)ACTIVE_COMPARATORParticipants with HER2-positive, unresectable LABC or MBC who have experienced disease progression after treatment with trastuzumab and a taxane will be treated with lapatinib plus capecitabine. Participants may continue to receive study treatment until disease progression (as assessed by the investigator), unmanageable toxicity, or study termination by the Sponsor.
Lapatinib + CapecitabineACTIVE_COMPARATORParticipants will receive lapatinib 1250 mg (five 250 mg tablets) orally once daily during each 21-day cycle + capecitabine 1000 milligrams per square meter (mg/m\^2) orally twice daily on Days 1-14 of each 21-day treatment cycle until PD (as assessed by the investigator), unmanageable toxicity, or study termination. Eligible participants will cross over to receive trastuzumab emtansine if second interim analysis demonstrates statistically significant overall survival benefit in favor of trastuzumab emtansine.

Interventions

NameTypeDescription
Trastuzumab EmtansineBIOLOGICALTrastuzumab emtansine 3.6 milligrams per kilogram (mg/kg) was administered intravenously on Day 1 of each 21-day cycle.
LapatinibDRUGLapatinib 1250 mg was administered orally once per day of each 21-day cycle.
CapecitabineDRUGCapecitabine 1000 milligrams per square meter (mg/m\^2) was administered orally twice daily on Days 1-14 of each 21-day cycle.
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites18

Inclusion Criteria: * Aged \>/= 18 years * Prospective centrally assessed HER2-positive disease (i.e., immunohistochemistry \[IHC\] 3+ and/or gene amplified \[HER2 to Chromosome 17 \[CEP 17\] ratio \>/= 2\]) by in situ hybridization (ISH) through use of archival paraffin-embedded tumor tissue * His...

Countries:ChinaUnited StatesBosnia and HerzegovinaBrazilBulgariaCanadaColombiaDenmarkFinlandFranceGermanyHong KongIndiaItalyMexicoNew ZealandPhilippinesPolandPortugalRussiaSingaporeSloveniaSouth KoreaSpainSwedenSwitzerlandTaiwanUnited Kingdom
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Competitive Landscape -Breast Cancer 402 trials

Top 20 of 92 competitors

CompanyTickerTrialsLead PhaseDrugs
AstraZeneca PLCAZN47PHASE3Fulvestrant, Capivasertib
Merck & Co., Inc.MRK12PHASE3Pembrolizumab, Paclitaxel, Doxorubicin, Epirubicin, Cyclophosphamide
Eli Lilly and CompanyLLY27PHASE3Abemaciclib, Standard Adjuvant Endocrine Therapy
BioNTech SE Sponsored ADRBNTX7PHASE3DB-1303/BNT323, T-DM1
Gilead Sciences, Inc.GILD13PHASE3Sacituzumab Govitecan-hziy, Eribulin, Capecitabine Product, Gemcitabine, Vinorelbine
Novartis AG Sponsored ADRNVS30PHASE3Ribociclib
Pfizer Inc.PFE34PHASE3ARV-471, Fulvestrant
BeOne Medicines Ltd. Sponsored ADRONC5PHASE3BGB-43395, Letrozole, Abemaciclib, Palbociclib, Ribociclib
Olema Pharmaceuticals, Inc.OLMA5PHASE3Palazestrant, Fulvestrant, Anastrozole, Letrozole, Exemestane
Jazz Pharmaceuticals Public Limited CompanyJAZZ3PHASE3Zanidatamab, Trastuzumab, Eribulin, Vinorelbine, Gemcitabine
Celcuity Inc.CELC3PHASE3Gedatolisib, Palbociclib, Fulvestrant, Alpelisib
Relay Therapeutics, Inc.RLAY2PHASE3Zovegalisib, Capivasertib, Fulvestrant
GSK plc Sponsored ADRGSK2PHASE3Niraparib
Greenwich LifeSciences, Inc.GLSI1PHASE3GLSI-100
Bristol-Myers Squibb CompanyBMY5PHASE2Iza-bren, Nab-paclitaxel, Paclitaxel, Capecitabine, Carboplatin
BriaCell Therapeutics CorpBCTX2PHASE3SV-BR-1-GM, Cyclophosphamide, Interferon infiltration of the inoculation site, Retifanlimab, Treatment of Physician's Choice
Incyte CorporationINCY4PHASE2Ruxolitinib, Capecitabine, Regorafenib
Natera, Inc.NTRA3PHASE2Discontinuation of the anti-HER2 maintenance therapy
Puma Biotechnology, Inc.PBYI3PHASE2Neratinib, Loperamide, Colesevelam
Atossa Therapeutics, Inc.ATOS1PHASE2endoxifen, goserelin
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Frequently asked questions about Lapatinib

What is Lapatinib used for in breast cancer?

Lapatinib is a small molecule being studied for the treatment of HER2-positive locally advanced or metastatic breast cancer. It is administered in combination with capecitabine in clinical trials. Lapatinib is an investigational drug and is not approved for this use.

How does Lapatinib work?

Lapatinib targets the HER2 receptor, which is overexpressed in certain breast cancers. By inhibiting HER2 signaling, it aims to slow or stop the growth of cancer cells. This mechanism is being evaluated in clinical trials for HER2-positive breast cancer.

Who is developing Lapatinib?

Lapatinib is being developed by Roche Holding AG, a company traded on the OTC market under the ticker RHHBY. Roche is conducting clinical trials to evaluate the drug's safety and efficacy in breast cancer.

What phase is Lapatinib in?

Lapatinib is in Phase 3 clinical development. Two Phase 3 trials have been completed, with a total of 1,342 participants enrolled. The drug remains investigational and has not been approved by regulatory authorities.

What clinical trials is Lapatinib in?

Lapatinib has been studied in two completed Phase 3 trials. NCT00829166 compared trastuzumab emtansine versus capecitabine plus lapatinib in 991 participants with HER2-positive locally advanced or metastatic breast cancer. NCT03084939 evaluated trastuzumab emtansine in 351 Chinese participants with the same condition.

Is Lapatinib the same as Tykerb?

Lapatinib is the generic name for the drug also known as Tykerb. In clinical trials, it is referred to as lapatinib, and it is being studied in combination with capecitabine for HER2-positive breast cancer.